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Human Pim-3 proto-oncogene, serine/threonine kinase (PIM family)
Assay data:8 Active, 8 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Human homeodomain interacting protein kinase 2 (HIPK subfamily)
Assay data:2 Active, 2 Tested
Human dual specificity tyrosine phosphorylation regulated kinase 3 (Dyrk2 subfamily)
Human casein kinase 2, alpha 1 polypeptide subunit (Casein kinase 2 (CK2) family)
Assay data:3 Active, 3 Tested
Inhibition of N-terminal His6X-tagged recombinant human full length casein kinase-2alpha expressed in SF21 cells using BODIPY-FL-RRRDDDSDDD-CONH2 as substrate preincubated for 20 mins measured after 90 mins by mobility shift assay
Assay data:28 Active, 28 Activity ≤ 1 µM, 28 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of casein kinase-2 in human HCT116 cells assessed as inhibition of AKT phosphorylation at Ser129 after 3 to 24 hrs by Western blot analysis
Assay data:17 Active, 17 Activity ≤ 1 µM, 21 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed Citation
Growth inhibition of human HCT116 cells after 72 hrs by Alamar blue assay
Assay data:23 Active, 23 Activity ≤ 1 µM, 25 Tested
Aqueous solubility of the compound in phosphate buffer at pH 7.4 after 24 hrs
Assay data:15 Active, 6 Activity ≤ 1 µM, 27 Tested
Binding affinity to human ERG expressed in CHO cells by IonWorks assay
Assay data:17 Tested
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of casein kinase-2 (unknown origin)
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Cmax in po dosed rat
Assay data:4 Active, 4 Activity ≤ 1 µM, 4 Tested
Inhibition of Hipk-2 (unknown origin)
Inhibition of PIM3 (unknown origin)
Inhibition of Dyrk-3 (unknown origin)
Inhibition of GSK3beta (unknown origin)
Assay data:1 Active, 1 Tested
Inhibition of CDK2 (unknown origin)
Octanol-water partition coefficient, log D of the compound at pH 7.4 after 5 hrs by shake-flask method
Assay data:26 Tested
SummaryPubMed Citation
Fraction unbound in human plasma at 10 uM by equilibrium dialysis method
Intrinsic clearance in rat liver microsomes
Assay data:27 Tested
Apparent permeability across apical to basolateral side in porcine LLC cells expressing MDR1
Assay data:1 Tested
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